An orally bioavailable mPGES-1 inhibitor (IC50 = 3 nM); selective for mPGES-1 over PGDS

PF-4693627 – 10 mg

Brand:
Cayman
CAS:
1312815-93-2
Storage:
-20
UN-No:
Non-Hazardous - /

PF-4693627 is an orally bioavailable inhibitor of microsomal prostaglandin E (PGE) synthase-1 (mPGES-1; IC50 = 3 nM).{40125} It is selective for mPGES-1 over PGDS, TXAS, and 5-LO in HWB-1483 cells, which have IC50 values greater than 50 μM, as well as COX-2 in fetal fibroblasts (IC50 = >10 μM). PF-4693627 inhibits LPS-stimulated synthesis of PGE2 in human whole blood (IC50 = 109 nM). In vivo, PF-4693627 (10 mg/kg) inhibits PGE2 production in a guinea pig model of carrageenan-induced air pouch inflammation.  

 

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Description

An orally bioavailable mPGES-1 inhibitor (IC50 = 3 nM); selective for mPGES-1 over PGDS, TXAS, and 5-LO in HWB-1483 cells, which have IC50 values >50 μM, as well as COX-2 in fetal fibroblasts (IC50 = >10 μM); inhibits LPS-stimulated synthesis of PGE2 in human whole blood (IC50 = 109 nM); inhibits PGE2 production in a guinea pig model of carrageenan-induced air pouch inflammation (10 mg/kg)

Formal name: 1-[5-chloro-6-(4-chlorophenyl)-2-benzoxazolyl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-4-piperidinecarboxamide

Synonyms: 

Molecular weight: 502.4

CAS: 1312815-93-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Prostaglandin Synthases||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Prostaglandins||Research Area|Lipid Biochemistry|Cyclooxygenase Pathway

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